"目录号: HY-14171
Metabolic Enzyme/ProteaseAutophagy-
Bexarotene (Targretin)是维甲酸X受体（RXR）激动剂，可作用于CTCL。
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生物活性
Description
Bexarotene (Targretin) is a selective RXR agonist approved for the treatment of CTCL.IC50 value:Target: retinoid X receptorExposure of NSCLC cell lines to bexarotene as a single agent had modest growth inhibitory effects (at > 1 μM). However, exposure of several NSCLC lines to bexarotene (1–3 μM) produced significant decreases in the expression of EGFR, Her-2 and TGF mRNA and protein. EGF levels were also decreased to a much lesser degree.
Clinical Trial
Dartmouth-Hitchcock Medical Center-Bristol-Myers Squibb-Ligand Pharmaceuticals
Carcinoma, Non-small-cell Lung
August 2001
Phase 1-Phase 2
Abramson Cancer Center of the University of Pennsylvania
Acute Myeloid Leukemia
January 2008
Phase 2
Georgetown University-Daiichi Sankyo Inc.
Solid Tumors-Lymphoma-Multiple Myeloma
December 2011
Phase 1
Dartmouth-Hitchcock Medical Center-Ligand Pharmaceuticals-Genentech, Inc.
Carcinoma, Non-small-cell Lung
December 2005
University of Virginia
Cushing's Disease
November 2008
Phase 1-Phase 2
The Cleveland Clinic
Alzheimer's Disease
February 2013
Phase 2
Dartmouth-Hitchcock Medical Center-Genentech, Inc.-Ligand Pharmaceuticals
Advanced, Malignant Aerodigestive Tract Tumor (Lung, Head and Neck and Esophagus)
April 2003
Phase 1
Baylor Breast Care Center-National Cancer Institute (NCI)
Breast Cancer
September 2001
Phase 1
Dartmouth-Hitchcock Medical Center-Ligand Pharmaceuticals-Genentech, Inc.
Carcinoma, Non-small-cell Lung
August 2005
Phase 2
ReXceptor, Inc.
Alzheimer's Disease
August 2014
Phase 1
Valeant Pharmaceuticals International, Inc.
Refractory Cutaneous T-cell Lymphoma
December 2009
Phase 4
University College, London
Lymphoma
March 2008
Phase 2
Washington University School of Medicine
Leukemia, Myeloid, Acute
May 2010
Phase 1
Abramson Cancer Center of the University of Pennsylvania
AML-Acute Myeloid Leukemia
January 2004
Phase 1
M.D. Anderson Cancer Center-United States Department of Defense
Lung Cancer
November 2006
Phase 2
Boston University-Ligand Pharmaceuticals
Cutaneous T-Cell Lymphoma
December 2001
Phase 1-Phase 2
Beersheva Mental Health Center
Schizophrenia
November 2008
Phase 3
Millennium Pharmaceuticals, Inc.-Seattle Genetics, Inc.-Takeda
Primary Cutaneous Anaplastic Large Cell Lymphoma-Mycosis Fungoides-Cutaneous T-Cell Lymphoma
August 2012
Phase 3
Memorial Sloan Kettering Cancer Center-National Cancer Institute (NCI)-Tibotec Pharmaceutical Limited-M.D. Anderson Cancer Center-New York University School of Medicine-Hackensack University Medical Center-Roswell Park Cancer Institute
Lymphoma
November 2005
Phase 2
Vanderbilt University
Cutaneous T-cell Lymphoma-Mycosis Fungoides-Sezary Syndrome
June 2005
Phase 2
Beersheva Mental Health Center-Stanley Medical Research Institute
Schizophrenia
September 2005
Phase 3
University of Medicine and Dentistry of New Jersey-Ligand Pharmaceuticals-Rutgers, The State University of New Jersey
Psoriasis
November 2003
Phase 2
Spectrum Pharmaceuticals, Inc
Cutaneous T-cell Lymphoma-Mycosis Fungoides-Sezary Syndrome-Primary Cutaneous Anaplastic Large Cell Lymphoma
March 2010
Phase 1
Fox Chase Cancer Center-Ligand Pharmaceuticals
Parapsoriasis
April 2001
Phase 2
Ligand Pharmaceuticals-National Cancer Institute (NCI)
Breast Cancer
October 1998
Phase 2
European Organisation for Research and Treatment of Cancer - EORTC
Lymphoma
January 2003
Phase 3
Merck Sharp & Dohme Corp.
Lymphoma
September 2005
Phase 1
University of Colorado, Denver-American Cancer Society, Inc.-Eisai Inc.
Thyroid Cancer
November 2008
Early Phase 1
Eisai Inc.
Non-small Cell Lung Cancer
May 2002
Phase 3
Eisai Inc.
Non-small Cell Lung Cancer
Phase 3
Stanford University-Ligand Pharmaceuticals-AstraZeneca
Lung Cancer
April 2004
Phase 1-Phase 2
Memorial Sloan Kettering Cancer Center-National Cancer Institute (NCI)
Lymphoma
October 2001
Phase 2
Beersheva Mental Health Center
Schizophrenia-Schizoaffective Disorder-Cognition
Phase 3
Ligand Pharmaceuticals-NIH AIDS Clinical Trials Information Service
Sarcoma, Kaposi-HIV Infections
Phase 2
Sidney Kimmel Comprehensive Cancer Center-National Cancer Institute (NCI)
Leukemia-Myelodysplastic Syndromes-Myelodysplastic/Myeloproliferative Diseases
November 2006
Phase 2
Raghu Nandan, M.D., Inc-National Cancer Institute (NCI)
Lung Cancer
January 2007
Phase 2
Millennix-National Cancer Institute (NCI)
Lymphoma
February 2001
Phase 2
Dartmouth-Hitchcock Medical Center-Bristol-Myers Squibb-Ligand Pharmaceuticals
Carcinoma, Non-small-cell Lung
August 2001
Phase 1-Phase 2
Abramson Cancer Center of the University of Pennsylvania
Acute Myeloid Leukemia
January 2008
Phase 2
Georgetown University-Daiichi Sankyo Inc.
Solid Tumors-Lymphoma-Multiple Myeloma
December 2011
Phase 1
Dartmouth-Hitchcock Medical Center-Ligand Pharmaceuticals-Genentech, Inc.
Carcinoma, Non-small-cell Lung
December 2005
University of Virginia
Cushing's Disease
November 2008
Phase 1-Phase 2
The Cleveland Clinic
Alzheimer's Disease
February 2013
Phase 2
Dartmouth-Hitchcock Medical Center-Genentech, Inc.-Ligand Pharmaceuticals
Advanced, Malignant Aerodigestive Tract Tumor (Lung, Head and Neck and Esophagus)
April 2003
Phase 1
Baylor Breast Care Center-National Cancer Institute (NCI)
Breast Cancer
September 2001
Phase 1
Dartmouth-Hitchcock Medical Center-Ligand Pharmaceuticals-Genentech, Inc.
Carcinoma, Non-small-cell Lung
August 2005
Phase 2
ReXceptor, Inc.
Alzheimer's Disease
August 2014
Phase 1
Valeant Pharmaceuticals International, Inc.
Refractory Cutaneous T-cell Lymphoma
December 2009
Phase 4
